Готові списки джерел за темами / Pleiotropic prodrugs

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Добірка наукової літератури з теми "Pleiotropic prodrugs"

Автор: Grafiati

Опубліковано: 21 грудня 2024

Оновлено: 31 липня 2025

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Статті в журналах з теми "Pleiotropic prodrugs"

Li, Jiaqi. "Advances and applications of prodrug strategies in drug design." Journal of Food Science, Nutrition and Health 3, no. 1 (2024): 12–22. https://doi.org/10.54254/3029-0821/3/2024023.

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Of all the drugs launched on the market over the past decade, a substantial number of approved prodrugs have been significant, underscoring the importance of this prodrug to drug design. It is reported that 10% of all marketed drugs globally can be classified as prodrugs. The core goal of the prodrug strategy is to improve the undesirable properties of the drug molecule, including but not limited to insufficient solubility, low selectivity, poor chemical stability, poor taste, strong local irritation, significant pain, and possible systemic toxicity during metabolism in vivo. This review artic

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Toublet, François-Xavier, Cédric Lecoutey, Julien Lalut, et al. "Inhibiting Acetylcholinesterase to Activate Pleiotropic Prodrugs with Therapeutic Interest in Alzheimer’s Disease." Molecules 24, no. 15 (2019): 2786. http://dx.doi.org/10.3390/molecules24152786.

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Alzheimer’s disease (AD) is a multifactorial neurodegenerative disease which is still poorly understood. The drugs currently used against AD, mainly acetylcholinesterase inhibitors (AChEI), are considered clinically insufficient and are responsible for deleterious side effects. AChE is, however, currently receiving renewed interest through the discovery of a chaperone role played in the pathogenesis of AD. But AChE could also serve as an activating protein for pleiotropic prodrugs. Indeed, inhibiting central AChE with brain-penetrating designed carbamates which are able to covalently bind to t

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Chirumbolo, Salvatore, Geir Bjørklund, Roman Lysiuk, Antonio Vella, Larysa Lenchyk, and Taras Upyr. "Targeting Cancer with Phytochemicals via Their Fine Tuning of the Cell Survival Signaling Pathways." International Journal of Molecular Sciences 19, no. 11 (2018): 3568. http://dx.doi.org/10.3390/ijms19113568.

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The role of phytochemicals as potential prodrugs or therapeutic substances against tumors has come in the spotlight in the very recent years, thanks to the huge mass of encouraging and promising results of the in vitro activity of many phenolic compounds from plant raw extracts against many cancer cell lines. Little but important evidence can be retrieved from the clinical and nutritional scientific literature, where flavonoids are investigated as major pro-apoptotic and anti-metastatic compounds. However, the actual role of these compounds in cancer is still far to be fully elucidated. Many o

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Campos-Salinas, Jenny, Margarita Barriga, and Mario Delgado. "Therapeutic Effect of a Latent Form of Cortistatin in Experimental Inflammatory and Fibrotic Disorders." Pharmaceutics 14, no. 12 (2022): 2785. http://dx.doi.org/10.3390/pharmaceutics14122785.

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Cortistatin is a cyclic neuropeptide that recently emerged as an attractive therapeutic factor for treating inflammatory, autoimmune, fibrotic, and pain disorders. Despite of its efficiency and apparent safety in experimental preclinical models, its short half-life in body fluids and its potential pleiotropic effects, due to its promiscuity for several receptors expressed in various cells and tissues, represent two major drawbacks for the clinical translation of cortistatin-based therapies. Therefore, the design of new strategies focused on increasing the stability, bioavailability, and target

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Toublet, François-Xavier, Julien Lalut, Bérénice Hatat, et al. "Pleiotropic prodrugs: Design of a dual butyrylcholinesterase inhibitor and 5-HT6 receptor antagonist with therapeutic interest in Alzheimer’s disease." European Journal of Medicinal Chemistry 210 (January 2021): 113059. http://dx.doi.org/10.1016/j.ejmech.2020.113059.

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Leitsch, David. "A review on metronidazole: an old warhorse in antimicrobial chemotherapy." Parasitology 146, no. 9 (2017): 1167–78. http://dx.doi.org/10.1017/s0031182017002025.

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AbstractThe 5-nitroimidazole drug metronidazole has remained the drug of choice in the treatment of anaerobic infections, parasitic as well as bacterial, ever since its development in 1959. In contrast to most other antimicrobials, it has a pleiotropic mode of action and reacts with a large number of molecules. Importantly, metronidazole, which is strictly speaking a prodrug, needs to be reduced at its nitro group in order to become toxic. Reduction of metronidazole, however, only takes place under very low concentrations of oxygen, explaining why metronidazole is exclusively toxic to microaer

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Bettendorff, Lucien. "Synthetic Thioesters of Thiamine: Promising Tools for Slowing Progression of Neurodegenerative Diseases." International Journal of Molecular Sciences 24, no. 14 (2023): 11296. http://dx.doi.org/10.3390/ijms241411296.

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Thiamine (vitamin B1) is essential for the brain. This is attributed to the coenzyme role of thiamine diphosphate (ThDP) in glucose and energy metabolism. The synthetic thiamine prodrug, the thioester benfotiamine (BFT), has been extensively studied and has beneficial effects both in rodent models of neurodegeneration and in human clinical studies. BFT has no known adverse effects and improves cognitive outcomes in patients with mild Alzheimer’s disease. In cell culture and animal models, BFT has antioxidant and anti-inflammatory properties that seem to be mediated by a mechanism independent o

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Nirschl, Christopher J., Pam Alderhold, Heather R. Brodkin, et al. "Abstract 2055: WTX-330 is a conditionally activated IL-12 prodrug that fundamentally reprograms tumor infiltrating CD8+ T cells and drives tumor regression." Cancer Research 82, no. 12_Supplement (2022): 2055. http://dx.doi.org/10.1158/1538-7445.am2022-2055.

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Abstract Immune checkpoint inhibition (ICI) has established immunotherapy as the first line of treatment in a subset of cancers. However, there are still many patients and cancer types where ICI is not effective, representing a significant unmet clinical need for novel immunotherapies to expand the clinical options for patients. Interleukin 12 (IL-12) is a pleiotropic cytokine that drives naïve T cells towards a TH1 phenotype, activates NK cells and cytotoxic T cells, and strongly induces the expression of IFNγ by multiple cell types, making it an attractive pro-inflammatory cytokine for cance

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Su, Qingtai, Stephen Gutowski, Austin Burcham, et al. "Abstract LB438: Preclinical characterization of ONM-412, an ultra-pH sensitive nanoparticle encapsulated IL-12 fusion protein." Cancer Research 84, no. 7_Supplement (2024): LB438. http://dx.doi.org/10.1158/1538-7445.am2024-lb438.

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Abstract Background: Interleukin-12 is a potent pleiotropic cytokine, but its clinical translation has been hindered by toxicities. To deliver IL-12 to tumors with high spatial and temporal precision while minimizing off-tumor effects, we have developed an ultra-pH sensitive nanoparticle platform - ON-BOARD - that shields payloads from systemic exposure and targets solid tumors by responding to tumor acidity. Herein, we report the preclinical efficacy and safety characterization of ONM-412, an ON-BOARD nanoparticle encapsulated IL-12Fc fusion protein, and muONM-412, an encapsulated murine IL-1

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Meden, Anže, Neža Žnidaršič, Damijan Knez, et al. "Pleiotropic prodrugs for both symptomatic and disease-modifying treatment of Alzheimer’s disease." Acta Pharmaceutica Sinica B, July 2025. https://doi.org/10.1016/j.apsb.2025.07.005.

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Більше джерел

Дисертації з теми "Pleiotropic prodrugs"

Toublet, Francois-Xavier. "Conception, synthèse et évaluation biologique de prodrogues pléiotropes d'intérêt dans la maladie d'Alzheimer." Thesis, Normandie, 2019. http://www.theses.fr/2019NORMC429.

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Анотація:

La maladie d’Alzheimer (MA) est une maladie neurodégénérative multifactorielle encore mal comprise. Les médicaments actuellement utilisés contre la MA, principalement des inhibiteurs de cholinestérases (IChE), sont considérés comme ayant un service médical rendu insuffisant et sont responsables d’effets secondaires délétères. Les ChE suscitent toutefois un regain d’intérêt grâce à la découverte du rôle de chaperon joué dans la pathogenèse de la MA. Ces enzymes pourraient également servir de protéine d'activation pour les promédicaments pléiotropes. En effet, l'inhibition des ChE centrales par

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Wang, Alice. "Cοnceptiοn, synthèse et évaluatiοn biοlοgique de nοuveaux prοmédicaments d'intérêt thérapeutique pοtentiel pοur le traitement de la maladie d'Alzheimer et du syndrοme de Dοwn assοcié". Electronic Thesis or Diss., Normandie, 2024. http://www.theses.fr/2024NORMC233.

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Анотація:

Des études ont montré que les personnes atteintes de syndrome de Down (SD) ou trisomie 21 présentent un risque plus élevé de développer une démence de type maladie d’Alzheimer (MA). En effet, certaines cibles thérapeutiques communes ont été retrouvées dans ces deux maladies multifactorielles, pour lesquelles aucun traitement efficace n’existe à l’heure actuelle. Afin de traiter simultanément ces origines communes, l'approche des ligands pléiotropes multi-cibles (MTDLs) semble prometteuse. Ces composés regroupent dans une structure unique plusieurs activités biologiques ciblant diverses causes

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